Scott, James S.; Birch, Alan M.; Brocklehurst, Katy J.; Broo, Anders; Brown, Hayley S.; Butlin, Roger J.; Clarke, David S.; Davidsson, Ojvind; Ertan, Anne; Goldberg, Kristin; Groombridge, Sam D.; Hudson, Julian A.; Laber, David; Leach, Andrew G.; MacFaul, Philip A.; McKerrecher, Darren; Pickup, Adrian; Schofield, Paul; Svensson, Per H.; Sorme, Pernilla; Teague, Joanne published the artcile< Use of Small-Molecule Crystal Structures To Address Solubility in a Novel Series of G Protein Coupled Receptor 119 Agonists: Optimization of a Lead and in Vivo Evaluation>, Recommanded Product: tert-Butyl 4-(5-bromopyrimidin-2-yl)piperazine-1-carboxylate, the main research area is antidiabetic GPCR119 agonist preparation structure activity crystal structure.
G protein coupled receptor 119 (GPR119) is viewed as an attractive target for the treatment of type 2 diabetes and other elements of the metabolic syndrome. During a program toward discovering agonists of GPR119, we herein describe optimization of an initial lead compound, 2, into a development candidate, 42. A key challenge in this program of work was the insolubility of the lead compound Small-mol. crystallog. was utilized to understand the intermol. interactions in the solid state and resulted in a switch from an aryl sulfone to a 3-cyanopyridyl motif. The compound was shown to be effective in wild-type but not knockout animals, confirming that the biol. effects were due to GPR119 agonism.
Journal of Medicinal Chemistry published new progress about 5-HT2B receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 374930-88-8 belongs to class piperazines, and the molecular formula is C13H19BrN4O2, Recommanded Product: tert-Butyl 4-(5-bromopyrimidin-2-yl)piperazine-1-carboxylate.
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